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Title:
NOVEL 2(S)-HYDROXY-3(S)-(4-ACYLOXYPHENYL)-3-(2- NITROPHENYLTHIO)-PROPIONIC ACIDS
Document Type and Number:
Japanese Patent JPS59196863
Kind Code:
A
Abstract:

NEW MATERIAL:A compound of formula I (R1 is acyl; R2 is H, lower alkyl) and its salt.

EXAMPLE: 2(S)-Hydroxy-3(S)-( 4-formyloxyphenyl )-3-( 2-nitrophenylthio ) propionic acid.

USE: A synthetic intermediate of diltiazem hydrochloride, which is a calcium antagonist.

PREPARATION: The addition of hydrochloric acid to a compound of formula IIis effected in a polar solvent such as acetonitrile, preferably in the presence of a weak-acid catalyst to furnish a compound of formula III as well as a small amount of a compound of formula III'. Then, the compound of formula III solely, or a mixture thereof with the compound of formula III' is dried under reduced pressure, dissolved in an organic solvent such as acetonitrile and allowed to react with a compound of formula IV in the presence of a base such as pyridine to give the compound of formula I .


Inventors:
HONMA TSUNETOSHI
IGARASHI KIKUO
Application Number:
JP7113983A
Publication Date:
November 08, 1984
Filing Date:
April 21, 1983
Export Citation:
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Assignee:
SHIONOGI SEIYAKU KK
International Classes:
C07D281/10; C07C67/00; C07C313/00; C07C323/62; (IPC1-7): C07C149/43; C07D281/10
Attorney, Agent or Firm:
Mitsutaka Iwasaki